[1S-[1R*(R*),2R*,4R*]]-[4-[[(3-氨基-2,2-二甲基-3-氧代丙基)氨基]羰基]-2-羟基-1-[2-[[4-甲氧基-3-(3-甲氧基丙氧基)苯基]甲基]-3-甲基丁基]-5-甲基己基]-氨基甲酸叔丁酯合成路线 （共 49 条）
反应条件
1: palladium 10 on activated carbon; triethylamine; hydrogen / ethyl acetate / 6 h / 20 °C
2: triethylamine; 2-hydroxy-pyridine / 36 h / 60 - 65 °C
View Scheme
参考文献
JUBILANT LIFE SCIENCES LIMITED; BISWAS, Sujay; SRIMURUGAN, Sankareswaran; KUMAR, Anjul; PANDA, Atulya, Kumar; JAMSHAD, Danish; MASAND, Mukesh; BISWAS, Bidyut; BANSAL, Vikas; GUPTA, Ashish, Kumar; VIR, Dharam
Patent: WO2013/61224 A1, 2013 ;
反应条件
1: 4-(N,N-dimethlyamino)pyridine; triethylamine / tetrahydrofuran / 24 h / 20 °C
2: triethylamine; 2-hydroxy-pyridine / tert-butyl methyl ether / 18 h / 80 °C
View Scheme
参考文献
CarboDesign LLC
Patent: US2011/105767 A1, 2011 ;
反应条件
1: triethylamine / dichloromethane / 5 °C
2: triethylamine; 2-hydroxy-pyridine
View Scheme
参考文献
DR. REDDY'S LABORATORIES LTD.; DR. REDDY'S LABORATORIES, INC.; KOLLA, Naveen Kumar; APPAYE, Kaliyaperumal Srinivasan; GANGULA, Srinivas; GOVINDAPUR, Rajeshwar Reddy; MANNE, Nagaraju; NIKUMBH, Satish Pandurang; NEELAM, Uday Kumar; JOSEPH, Suju Chuttippari; BADDAM, Sudhakar Reddy; KUNHIMON, Shyam Kumar Unniaranpurakkal; MOOVENDAN, Mohan; DAHANUKAR, Vilas; DONIPARTHI, Kiran Kumar
Patent: WO2012/21446 A2, 2012 ;
反应条件
1.1: hydrogenchloride / methanol / 2 h / 50 - 55 °C
1.2: pH 10.5 - 11
2.1: triethylamine / dichloromethane / 3 h / 20 °C
3.1: triethylamine; 2-hydroxy-pyridine / 36 h / 60 - 65 °C
View Scheme
参考文献
JUBILANT LIFE SCIENCES LIMITED; BISWAS, Sujay; SRIMURUGAN, Sankareswaran; KUMAR, Anjul; PANDA, Atulya, Kumar; JAMSHAD, Danish; MASAND, Mukesh; BISWAS, Bidyut; BANSAL, Vikas; GUPTA, Ashish, Kumar; VIR, Dharam
Patent: WO2013/61224 A1, 2013 ;
反应条件
1: palladium 10 on activated carbon; triethylamine; hydrogen / ethyl acetate / 6 h / 20 °C
2: triethylamine; 2-hydroxy-pyridine / 36 h / 60 - 65 °C
View Scheme
参考文献
JUBILANT LIFE SCIENCES LIMITED; BISWAS, Sujay; SRIMURUGAN, Sankareswaran; KUMAR, Anjul; PANDA, Atulya, Kumar; JAMSHAD, Danish; MASAND, Mukesh; BISWAS, Bidyut; BANSAL, Vikas; GUPTA, Ashish, Kumar; VIR, Dharam
Patent: WO2013/61224 A1, 2013 ;
反应条件
1.1: 5 palladium on charcoal; hydrogen / methanol / 12 h / 20 °C
2.1: methanol / 1 h / 20 °C
3.1: triethylsilane / dichloromethane / 20 °C
3.2: -78 - -75 °C
4.1: hydrogenchloride / methanol / 2 h / 50 - 55 °C
4.2: pH 10.5 - 11
5.1: triethylamine / dichloromethane / 3 h / 20 °C
6.1: triethylamine; 2-hydroxy-pyridine / 36 h / 60 - 65 °C
View Scheme
参考文献
JUBILANT LIFE SCIENCES LIMITED; BISWAS, Sujay; SRIMURUGAN, Sankareswaran; KUMAR, Anjul; PANDA, Atulya, Kumar; JAMSHAD, Danish; MASAND, Mukesh; BISWAS, Bidyut; BANSAL, Vikas; GUPTA, Ashish, Kumar; VIR, Dharam
Patent: WO2013/61224 A1, 2013 ;
反应条件
1.1: methanol / 1 h / 20 °C
2.1: triethylsilane / dichloromethane / 20 °C
2.2: -78 - -75 °C
3.1: hydrogenchloride / methanol / 2 h / 50 - 55 °C
3.2: pH 10.5 - 11
4.1: triethylamine / dichloromethane / 3 h / 20 °C
5.1: triethylamine; 2-hydroxy-pyridine / 36 h / 60 - 65 °C
View Scheme
参考文献
JUBILANT LIFE SCIENCES LIMITED; BISWAS, Sujay; SRIMURUGAN, Sankareswaran; KUMAR, Anjul; PANDA, Atulya, Kumar; JAMSHAD, Danish; MASAND, Mukesh; BISWAS, Bidyut; BANSAL, Vikas; GUPTA, Ashish, Kumar; VIR, Dharam
Patent: WO2013/61224 A1, 2013 ;
反应条件
1.1: triethylsilane / dichloromethane / 20 °C
1.2: -78 - -75 °C
2.1: hydrogenchloride / methanol / 2 h / 50 - 55 °C
2.2: pH 10.5 - 11
3.1: triethylamine / dichloromethane / 3 h / 20 °C
4.1: triethylamine; 2-hydroxy-pyridine / 36 h / 60 - 65 °C
View Scheme
参考文献
JUBILANT LIFE SCIENCES LIMITED; BISWAS, Sujay; SRIMURUGAN, Sankareswaran; KUMAR, Anjul; PANDA, Atulya, Kumar; JAMSHAD, Danish; MASAND, Mukesh; BISWAS, Bidyut; BANSAL, Vikas; GUPTA, Ashish, Kumar; VIR, Dharam
Patent: WO2013/61224 A1, 2013 ;
反应条件
1: 38 percent / TPAP; NMMO
2: 65 percent / 2-hydroxypyridine; Et3N
View Scheme
参考文献
Dong, Hua; Zhang, Zhi-Liu; Huang, Jia-Hui; Ma, Rujian; Chen, Shu-Hui; Li, Ge
Tetrahedron Letters, 2005 , vol. 46, # 37 p. 6337 - 6340
